Synthesis and cytotoxic evaluation of heterocyclic compounds by vinylic substitution of ketene dithioacetals.

N-heterocyclic compounds are important molecular scaffolds in the search for new drugs, since most drugs contain heterocyclic moieties in their molecular structure, and some of these classes of heterocycles are able to provide ligands for two or more biological targets. Ketene dithioacetals are important building blocks in organic synthesis and are widely used in the synthesis of N-heterocyclic compounds. In this work, we used double vinylic substitution reactions on ketene dithioacetals to synthesize a small library of heterocyclic derivatives and evaluated their cytotoxic activity in breast and ovarian cancer cells, identifying two benzoxazoles with good potency and selectivity. In silico predictions indicate that the two most active derivatives exhibit physicochemical properties within the range of drug-like compounds and showed potential to interact with HDAC8 and ERK1 cancer-related targets.

miR-197, miR-26a and miR-27a analysis in chronic lymphocytic leukemia.

Aims: Chronic lymphocytic leukemia (CLL) involves the proliferation and increase of B-lymphocytes in the peripheral blood, bone marrow and lymphoid organs. This study evaluated the microRNAs miR-197, miR-26a and miR-27a as potential biomarkers for CLL. Patients & Methods: Eighty-two patients with CLL and 62 control subjects (CT) were investigated for these targets, using quantitative PCR (qPCR). Results: A significant reduction of all microRNAs was observed in CLL compared to the controls (p < 0.001). Significant negative correlations were observed for the clinical staging groups. After adjusting for multiple logistic regression analysis, miR-197 and miR-26a remained as possible independent risk factors related to the CLL. Conclusions: Our data indicated good performance of this microRNAs as potential biomarkers in CLL.